Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Aqueous film coating solution, film coated granule and tablet using the same

a film coating solution and film coating technology, applied in the direction of powder delivery, inks, microcapsules, etc., can solve the problems of drug release control performance and acid resistance required to the film layer that are often deteriorated, and achieve good acid resistance, good acid resistance, and sustained release properties

Active Publication Date: 2010-10-14
ASAHI KASEI CHEM CORP
View PDF9 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to an aqueous film coating solution for pharmaceutical preparations, particularly tablets and granules. The technical effects of the invention include improving the performance uniformity and sustained release properties of tablets and granules, as well as enhancing the acid resistance of enteric film coatings. The invention also addresses the issue of damaging the film layer during tablet compression force and provides a solution to improve the hardness and handleability of tablets. Additionally, the invention provides a method for producing a sustained release tablet with improved acid resistance and sustained release properties.

Problems solved by technology

However, when tableting a film coated granule by the compression molding, the film layer (coating layer) is damaged by the pressure applied at the time of the compression molding, whereby the drug release-control performance and acid resistance required to the film layer are often deteriorated.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Aqueous film coating solution, film coated granule and tablet using the same
  • Aqueous film coating solution, film coated granule and tablet using the same
  • Aqueous film coating solution, film coated granule and tablet using the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Elementary Granule

[0074]20.0 kg of a crystalline cellulose spherical nuclear particle (tradename: CELPHERE CP-305, average particle size: 385 μm, Asahi Kasei Chemicals Corporation) was placed in a tumbling fluidized bed coater (Multiplex MP-25 model, Powlex Corporation). Using 10 mass % of riboflavin (Daiichi Fine Chemical Co., Ltd.) as a drug, 3 mass % of povidone (PVP-K30, ISP Ltd.) as a binder and a layering solution composed of 87 mass % of purified water, the above nuclear particles were subjected to the layering under the following conditions. The thus obtained layered particles were sieved using a sieve having an opening of 600 μm, and 20.35 kg of an elementary granule [G1] which passed through the sieve with the opening was obtained.

(1)Air supply temperature:75°C.(2)Air discharge temperature:40 to 45°C.(3)Air flow volume:8.0m3 / min(4)Number of rotor rotation:240rpm(5)Spray air supply pressure:0.6MPa(6)Spray air volume:400N / min(7)Spray nozzle size:2.2mm(8)Amount...

example 2

[0082]By the following formula, an aqueous film coating solution [L2] was prepared wherein an ethyl acrylate / methyl methacrylate copolymer dispersion [a], a methacrylic acid copolymer LD dispersion [b], a triethyl citrate [c], a titanium oxide [d], a methacrylic acid copolymer L [e] and purified water were contained in a solid content of 17 mass %.

[0083]Eudragit L100 (Degussa) was crushed to an average particle size of 20 μm using a jet mill pulverizer to use as the methacrylic acid copolymer L [e], and the same materials as in Example 1 were used as other components [a] to [d]. The solid mass ratio of these components was a:b:c:d:e=45:30:5:10:10 (=100:66.7:11.1:22.2:22.2). The tensile elongation of the cast film formed using the aqueous film coating solution [L2] was 213%.

[0084]Next, a film coated granule [F2] was produced in the same manner as in Example 1 except that the aqueous film coating solution [L2] was used in place of the aqueous film coating solution [L1].

[0085]The coate...

example 3

[0089]A film coating solution [L3] having a solid content of 17 mass % was prepared in the same manner as in Example 1 except that the solid mass ratio of the blending components was a:b:c:d=60:25:7.5:7.5 (=100:41.6:12.5:12.5). The tensile elongation of the aqueous film coating solution [L3] was 443%.

[0090]Next, a film coated granule [F3] was produced in the same manner as in Example 1 except that the aqueous film coating solution [L3] was used in place of the aqueous film coating solution [L1].

[0091]The coated film amount of the obtained film coated granule [F3] was 20 mass %, and the average particle size was 454 μm (the film thickness was about 25.8 μm). The yield was 92.8% and the agglomeration rate (the ratio of coarse particles of 600 μm or larger) was 10.2%.

[0092]The film coated granule [F3] had riboflavin dissolution rates of 0.7% in the 1st fluid after 3 hours and 26.3% in the 2nd fluid after 2 hours, 61.5% after 4 hours and 75.3% after 6 hours, 83.6% after 8 hours and 89.6...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

An object of the present invention is to provide an aqueous film coating solution, and the like, which has good acid resistance and sustained release properties as well as the flexibility suitable for the tablet compression force and are highly productive and cost efficient. The aqueous film coating solution of the present invention comprises an ethyl acrylate / methyl methacrylate copolymer dispersion, a methacrylic acid copolymer LD, a plasticizer, titanium oxide and water, wherein the solid mass ratio of the ethyl acrylate / methyl methacrylate copolymer dispersion, the methacrylic acid copolymer LD, the plasticizer and the titanium oxide is 100:(40 to 100):(5 to 50):(5 to 30) and the solid content thereof is 5 to 20 mass %.

Description

TECHNICAL FIELD[0001]The present invention relates to aqueous film coating solutions and film coated granules as well as tablets using the same and, in particular, to an aqueous film coating solution preferably used for the purpose of pharmaceutical preparations.BACKGROUND ART[0002]In the pharmaceutical solid preparations, a sustained release film coating may sometimes be used for the purpose of reducing adverse drug reactions, reducing the dose frequency and enhancing drug effects. In another case, in the oral preparations containing a drug which degrades in a low pH environment, the preparations may be coated with an enteric film for the purpose of protecting the drug from the gastric acid. Accordingly, to sustained release the preparation containing a drug unstable in a low pH environment, it is essential to impart both functions of the protection from the gastric acid and the sustained release properties.[0003]This type of film coating is commonly applied to tablets and granules...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/717C08K3/22C08K5/11C08K5/05C08K5/12A61K9/16A61K9/20
CPCA61K9/2081A61K9/5026A61K9/2846
Inventor YOSHIDA, NAOYAYAGINUMA, YOSHIHITO
Owner ASAHI KASEI CHEM CORP
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com